Filgotinib

• Description:

  Filgotinib (GLPG0634) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib can effectively inhibit the activities of JAK1, JAK2, JAK3 and TYK2 with IC50 values of 10 nM, 28 nM, 810 nM and 116 nM, respectively. Filgotinib also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib can be used in the study of rheumatoid arthritis and inflammatory bowel disease[1][2][3].

• Product Name Alternative:

  GLPG0634

• UNSPSC:

  12352005

• Hazard Statement:

  H302, H315, H319, H335

• Target:

  HIV; JAK

• Type:

  Reference compound

• Related Pathways:

  Anti-infection; Epigenetics; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/GLPG0634.html

• Purity:

  99.44

• Solubility:

  DMSO : 25 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL

• Smiles:

  O=C (C1CC1) NC2=NN3C (C4=CC=C (CN5CCS (CC5) (=O) =O) C=C4) =CC=CC3=N2

• Molecular Formula:

  C21H23N5O3S

• Molecular Weight:

  425.50

• Precautions:

  H302, H315, H319, H335

• References & Citations:

  [1]Van Rompaey L, et al. Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. J Immunol. 2013, 191 (7), 3568-3577.|[2]Menet CJ, et al. Triazolopyridines as Selective JAK1 Inhibitors: From Hit Identification to GLPG0634. J Med Chem. 2014 Nov 17.|[3]Yeh, et al. "Filgotinib suppresses HIV-1–driven gene transcription by inhibiting HIV-1 splicing and T cell activation." The Journal of Clinical Investigation 130.9 (2020) : 4969-4984.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Launched

• Isoform:

  JAK1; JAK2; JAK3; Tyk2

• CAS Number:

  1206161-97-8